Bazedoxifene

Information about Bazedoxifene

Bazedoxifene (ba" ze dox' i feen) is a selective estrogen receptor modulator that is used to prevent osteoporosis in menopausal women and for treatment of moderate-to-severe vasomotor symptoms associated with menopause (hot flashes, sweating).

Mechanism of action of Bazedoxifene

Bazedoxifene has estrogen-like effects (agonism) on bone and the cardiovascular system, but antiestrogen activity (antagonism) on breast and uterus tissue. This differential activity is keyed to achieving the beneficial effects of estrogens on bone in decreasing bone resorption and turnover and thus preventing osteoporosis, but avoiding the potential harmful effects of estrogen stimulation of breast and uterine tissue.

FDA approval information for Bazedoxifene

While bazedoxifene by itself is approved for use in several other countries of the world, in the United States it is approved only as a combination product with low doses of conjugated estrogens. In short term trials the combination of bazedoxifene and estrogens was shown to decrease menopause associated hot flushes. Longer term trials of this combination have documented its efficacy in preventing osteoporosis in postmenopausal women. The fixed combination of bazedoxifene (20 mg) and conjugated estrogens (0.45 mg) was approved for use in the United States under the brand name Duavee in 2013.

Side effects of Bazedoxifene

Common side effects include muscle spasms, nausea, diarrhea, dyspepsia, dizziness and abdominal, throat and neck pain. Potential long term, severe adverse events include deep venous thrombosis, pulmonary embolism and ischemic strokes and the possible long term effects of estrogens such as increased risk of breast, endometrial and ovarian cancer and gallbladder disease.

Obstetrical and Gynecological Agents

• Emergency contraceptive agents
  • Levonorgestrel, Ulipristal

• Estrogens and Oral contraceptives

• • Selective estrogen receptor modulators
    • Bazedoxifene, Ospemifene, Raloxifene
  • Infertility agents

• Antiestrogens
  • Clomiphene, Letrozole, Tamoxifen

• Gonadotropins
  • Chorionic gonadotropin, Follicle stimulating hormone, Luteinizing hormone, Human gonadotropin releasing hormone

• Pregnancy termination agents
  • Mifepristone
• Progesterone and the Progestins

• Dailymed label info on Bazedoxifene
• FDA Bazedoxifene

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  Bazedoxifene
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  Bazedoxifene